WO2020086533A1 - 5-membered heteroaryl carboxamide compounds for treatment of hbv - Google Patents

5-membered heteroaryl carboxamide compounds for treatment of hbv Download PDF

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Publication number
WO2020086533A1
WO2020086533A1 PCT/US2019/057362 US2019057362W WO2020086533A1 WO 2020086533 A1 WO2020086533 A1 WO 2020086533A1 US 2019057362 W US2019057362 W US 2019057362W WO 2020086533 A1 WO2020086533 A1 WO 2020086533A1
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WO
WIPO (PCT)
Prior art keywords
methyl
mmol
amino
chloro
pyrazole
Prior art date
Application number
PCT/US2019/057362
Other languages
English (en)
French (fr)
Inventor
Simon Nicolas Haydar
Leping Li
Mark G. BURES
Roopa Rai
Lynne BANNEN
Michael Walker
Original Assignee
Assembly Biosciences, Inc.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority to AU2019364352A priority Critical patent/AU2019364352A1/en
Priority to KR1020217015135A priority patent/KR20210095143A/ko
Priority to EP19805797.8A priority patent/EP3870296A1/en
Priority to US17/287,681 priority patent/US11560370B1/en
Application filed by Assembly Biosciences, Inc. filed Critical Assembly Biosciences, Inc.
Priority to CN201980082985.8A priority patent/CN113195055A/zh
Priority to SG11202104086PA priority patent/SG11202104086PA/en
Priority to MX2021004580A priority patent/MX2021004580A/es
Priority to JP2021547054A priority patent/JP2022508953A/ja
Priority to EA202191109A priority patent/EA202191109A1/ru
Priority to BR112021007602-6A priority patent/BR112021007602A2/pt
Priority to CA3117449A priority patent/CA3117449A1/en
Publication of WO2020086533A1 publication Critical patent/WO2020086533A1/en
Priority to IL282433A priority patent/IL282433A/en
Priority to PH12021550887A priority patent/PH12021550887A1/en
Priority to US17/989,237 priority patent/US20240150324A1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/38—Nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/08—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing alicyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/08—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing alicyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/08—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing alicyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/08—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing alicyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
PCT/US2019/057362 2018-10-22 2019-10-22 5-membered heteroaryl carboxamide compounds for treatment of hbv WO2020086533A1 (en)

Priority Applications (14)

Application Number Priority Date Filing Date Title
SG11202104086PA SG11202104086PA (en) 2018-10-22 2019-10-22 5-membered heteroaryl carboxamide compounds for treatment of hbv
EP19805797.8A EP3870296A1 (en) 2018-10-22 2019-10-22 5-membered heteroaryl carboxamide compounds for treatment of hbv
US17/287,681 US11560370B1 (en) 2018-10-22 2019-10-22 5-membered heteroaryl carboxamide compounds for treatment of HBV
JP2021547054A JP2022508953A (ja) 2018-10-22 2019-10-22 Ｈｂｖの処置のための５員のヘテロアリールカルボキサミド化合物
CN201980082985.8A CN113195055A (zh) 2018-10-22 2019-10-22 用于hbv治疗的5元杂芳基甲酰胺化合物
KR1020217015135A KR20210095143A (ko) 2018-10-22 2019-10-22 Hbv의 치료를 위한 5원 헤테로아릴 카르복스아미드 화합물
MX2021004580A MX2021004580A (es) 2018-10-22 2019-10-22 Compuestos de heteroarilcarboxamida de 5 miembros para el tratamiento del vhb.
AU2019364352A AU2019364352A1 (en) 2018-10-22 2019-10-22 5-membered heteroaryl carboxamide compounds for treatment of HBV
EA202191109A EA202191109A1 (ru) 2019-06-07 2019-10-22 Соединения 5-членного гетероарилкарбоксамида для лечения вируса гепатита в
BR112021007602-6A BR112021007602A2 (pt) 2018-10-22 2019-10-22 compostos de heteroaril carboxamida de 5 membros para tratamento de hbv
CA3117449A CA3117449A1 (en) 2018-10-22 2019-10-22 5-membered heteroaryl carboxamide compounds for treatment of hbv
IL282433A IL282433A (en) 2018-10-22 2021-04-19 Heteroarylcarboxamide compounds with a pentameric heteroaryl ring for the treatment of HBV
PH12021550887A PH12021550887A1 (en) 2018-10-22 2021-04-21 5-membered heteroaryl carboxamide compounds for treatment of hbv
US17/989,237 US20240150324A1 (en) 2018-10-22 2022-11-17 5-Membered Heteroaryl Carboxamide Compounds for Treatment of HBV

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201862748906P 2018-10-22 2018-10-22
US62/748,906 2018-10-22
US201962858790P 2019-06-07 2019-06-07
US62/858,790 2019-06-07

Related Child Applications (2)

Application Number Title Priority Date Filing Date
US17/287,681 A-371-Of-International US11560370B1 (en) 2018-10-22 2019-10-22 5-membered heteroaryl carboxamide compounds for treatment of HBV
US17/989,237 Continuation US20240150324A1 (en) 2018-10-22 2022-11-17 5-Membered Heteroaryl Carboxamide Compounds for Treatment of HBV

Publications (1)

Publication Number Publication Date
WO2020086533A1 true WO2020086533A1 (en) 2020-04-30

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PCT/US2019/057362 WO2020086533A1 (en) 2018-10-22 2019-10-22 5-membered heteroaryl carboxamide compounds for treatment of hbv

Country Status (15)

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US (2) US11560370B1 (ko)
EP (1) EP3870296A1 (ko)
JP (1) JP2022508953A (ko)
KR (1) KR20210095143A (ko)
CN (1) CN113195055A (ko)
AU (1) AU2019364352A1 (ko)
BR (1) BR112021007602A2 (ko)
CA (1) CA3117449A1 (ko)
IL (1) IL282433A (ko)
MA (1) MA53983A (ko)
MX (1) MX2021004580A (ko)
PH (1) PH12021550887A1 (ko)
SG (1) SG11202104086PA (ko)
TW (1) TW202028190A (ko)
WO (1) WO2020086533A1 (ko)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021216642A1 (en) * 2020-04-22 2021-10-28 Assembly Biosciences, Inc. Pyrazole carboxamide compounds for treatment of hbv
WO2023067517A1 (en) * 2021-10-20 2023-04-27 Assembly Biosciences, Inc. Novel crystalline forms
WO2023069547A1 (en) * 2021-10-20 2023-04-27 Assembly Biosciences, Inc. 5-membered heteroaryl carboxamide compounds for treatment of hbv
WO2023105481A1 (en) * 2021-12-10 2023-06-15 Assembly Biosciences, Inc. Pharmaceutical compositions for the treatment of hbv

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111205264A (zh) * 2020-02-25 2020-05-29 成都睿智化学研究有限公司 一种合成同位羟基和甲磺酰甲基化合物的新方法

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Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021216642A1 (en) * 2020-04-22 2021-10-28 Assembly Biosciences, Inc. Pyrazole carboxamide compounds for treatment of hbv
WO2023067517A1 (en) * 2021-10-20 2023-04-27 Assembly Biosciences, Inc. Novel crystalline forms
WO2023069547A1 (en) * 2021-10-20 2023-04-27 Assembly Biosciences, Inc. 5-membered heteroaryl carboxamide compounds for treatment of hbv
WO2023105481A1 (en) * 2021-12-10 2023-06-15 Assembly Biosciences, Inc. Pharmaceutical compositions for the treatment of hbv

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KR20210095143A (ko) 2021-07-30
US11560370B1 (en) 2023-01-24
CA3117449A1 (en) 2020-04-30
AU2019364352A1 (en) 2021-06-03
MX2021004580A (es) 2021-09-08
EP3870296A1 (en) 2021-09-01
TW202028190A (zh) 2020-08-01
SG11202104086PA (en) 2021-05-28
PH12021550887A1 (en) 2022-02-21
US20240150324A1 (en) 2024-05-09
BR112021007602A2 (pt) 2021-07-27
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MA53983A (fr) 2021-12-15

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